Drug intelligence / Profile preview

lopinavir + ritonavir + xiyanping

Development stage
Unknown
Lead developer
AbbVie
Modality
Peptides, Small Molecules, Recombinant Proteins and Enzymes
Administration
Oral, Intravenous
01

Overview

Lopinavir + ritonavir + xiyanping is a combination therapy consisting of two antiretroviral drugs (lopinavir and ritonavir) and a traditional Chinese medicine (xiyanping). Lopinavir and ritonavir are both protease inhibitors used primarily in the treatment of HIV infection. Ritonavir acts as a pharmacokinetic enhancer by inhibiting CYP3A-mediated metabolism of lopinavir, thereby increasing its plasma concentration[1][4][7][8]. Xiyanping is an injectable preparation derived from andrographolide sulfonate with reported antiviral, anti-inflammatory, immune-regulating, and antipyretic effects. It has been widely used in China for respiratory infections such as bronchitis and hand-foot-mouth disease[5]. During the COVID-19 pandemic, this combination was explored for potential benefit due to the antiviral properties of all three components; however, herb-drug interactions have been observed—xiyanping can inhibit CYP3A4 activity noncompetitively in vitro and alter the pharmacokinetics of lopinavir/ritonavir[2][3]. The mechanism of action for this combination includes inhibition of HIV-1 protease (by lopinavir), boosting drug levels via CYP3A inhibition (by ritonavir), and modulation of inflammatory pathways including IL-17/Toll-like receptor/PI3K-Akt/JAK-STAT signaling by xiyanping[6].

Brand names
Kaletra
Other names
lopinavir and ritonavirLPV/RTVXYPxiyanping injection
02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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